TABLE 3

Region 2 SAR studies

Embedded ImageRHα4β2 nAChRsHα3β4 nAChRs
IC50 Value (μM)anHIC50 Value (μM)anH
KAB-18Embedded Image13.5 (9.7–18.5)−0.7NA
DDR-1Embedded Image25.5 (17.2–37.7)−1.113.2 (6.4–27.3)−0.6
DDR-2Embedded Image10.6 (3.5–32.1)−0.719.5 (6.7–56.9)−0.6
KAB-21Embedded Image6.3 (1.9–20.9)−0.918.5 (7.3–46.2)−0.7
DDR-19Embedded Image2.8 (1.3–6.1)−0.94.3 (1.6–11.4)−0.9
KAB-24Embedded Image8.0 (4.2–15.3)−1.25.5 (1.7–17.4)−0.9
KAB-22Embedded Image9.4 (5.5–16.1)−1.323.1 (11.1–48.2)−1.2
KAB-23Embedded Image7.9 (4.9–12.7)−0.712.1 (8.1–17.9)−0.9
KAB-19Embedded Image5.5 (2.0–15.2)−1.14.3 (1.0–17.7)−0.9
KAB-20Embedded Image6.0 (4.4–8.2)−1.55.9 (4.1–8.4)−0.8
KAB-30Embedded Image4.9 (2.5–9.5)−1.55.0 (3.0–8.3)−1.3
IB-2Embedded Image10.5 (7.4–14.8)−0.810.9 (5.1–23.3)−0.9
  • nH, Hill coefficient; NA, no activity at concentrations up to 100 μM.

  • a Values represent geometric means (confidence limits), n = 4–8.